Name | strontium ranelate |
Synonyms | StrontiuM Ranelic STRONCIUM RANELATE Ranelate StrontiuM strontium ranelate Distrontium renelate Ranelic acid strontium salt StrontiuM ranelate (Protelos) StrontiuM ranelate SynonyMs DistrontiuM renelate 5-[bis(carboxymethyl)amino]-3-(carboxymethyl)-4-cyanothiophene-2-carboxylic acid 5-[Bis(carboxymethyl)amino]-2-carboxy-4-cyano-3-thiopheneacetic acid strontium salt StrontiuM 2,2'-((5-carboxylato-4-(carboxylatoMethyl)-3-cyanothiophen-2-yl)azanediyl)diacetate 2-[N,N-Di(carboxymethyl)amino]-3-cyano-4-carboxymethylthiophene-5-carboxylic acid strontium salt 2,2'-((5-Carboxy-4-(carboxyMethyl)-3-cyanothiophen-2-yl)azanediyl)diacetic acid, distrontiuM salt |
CAS | 135459-87-9 |
EINECS | 690-882-9 |
InChI | InChI=1/C12H10N2O8S.7H2O.2Sr/c13-2-6-5(1-7(15)16)10(12(21)22)23-11(6)14(3-8(17)18)4-9(19)20;;;;;;;;;/h1,3-4H2,(H,15,16)(H,17,18)(H,19,20)(H,21,22);7*1H2;;/q;;;;;;;;2*+2/p-4 |
Molecular Formula | C12H6N2O8SSr2 |
Molar Mass | 513.491 |
Melting Point | >310°C (dec.) |
Boling Point | 778.8℃ at 760 mmHg |
Solubility | H2O: soluble1mg/mL, clear (warmed) |
Appearance | Crystalline solid |
Color | white to beige |
Storage Condition | Inert atmosphere,Store in freezer, under -20°C |
Physical and Chemical Properties |
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Use | Mainly for the treatment and prevention of postmenopausal women with osteoporosis, significantly reduce the risk of vertebral fractures and hip fractures. |
In vivo study | Strontium Ranelate increases bone formation and decreased bone resorption, which results in increased bone mass in the vertebrae of intact adult mice. In intact adult rats, Strontium Ranelate also increases bone mass, as measured by dual-energy X-ray absorptiometry, in lumbar vertebra and femur, and this is confirmed by histological assessment of trabecular bone volume in the tibial metaphysis. Strontium Ranelate is found to decrease bone resorption and to increase bone formation in alveolar bone in normal adult monkeys (Macaca fascicularis), which exhibits extensive bone remodeling. In ovariectomized rats, short-term (3 months) treatment with Strontium Ranelate prevents trabecular bone loss induced by oestrogen deficiency, as demonstrated by bone ash, bone mineral content and histomorphometric analysis in the tibial metaphysis. This effect results from decreased bone resorption while bone formation was maintained. These beneficial effects of Strontium Ranelate on bone mass and microarchitecture in ovariectomized rats are confirmed in long-term experiments. In this long-term study (2 years), the increase in bone mass and microarchitecture induced by Strontium Ranelate results in a marked improvement in bone strength, supporting the beneficial effect of this drug on bone resistance. |
Hazard Symbols | Xn - Harmful |
Risk Codes | 20/21/22 - Harmful by inhalation, in contact with skin and if swallowed. |
Safety Description | 36/37 - Wear suitable protective clothing and gloves. |
UN IDs | 3077 |
WGK Germany | 3 |
RTECS | XM7581000 |
HS Code | 29349990 |
Osteoporosis drug | Strontium ranelate is a drug for the treatment of osteoporosis. Its appearance is white to yellowish powder or crystalline powder. It is odorless, slightly soluble in water, almost insoluble in ethanol, and easily soluble in dilute hydrochloric acid. It was developed by French Servier Company. It was first listed in Ireland in November 2004 and in the UK in December of the same year. Japan Fujisawa Pharmaceutical Company has the right to develop, produce and sell this product in Japan. Clinically, it is mainly used to treat and prevent osteoporosis in postmenopausal women, and significantly reduce the risk of vertebral fracture and hip fracture. strontium ranelate has dual pharmacological effects of inhibiting bone resorption and promoting bone formation. On the one hand, it can increase the synthesis of collagen and non-collagen in osteoblast-enriched cells, and promote osteoblast-mediated bone formation by enhancing the proliferation of pre-osteoblasts. On the other hand, by reducing the osteoclast differentiation and reabsorption activity, reduce bone resorption, so that bone renewal to achieve balance, conducive to bone formation. Strontium ranelate mainly exerts its pharmacological effects through strontium atoms. Strontium is an alkaline earth metal element of the same family as calcium, which is located below calcium in the periodic table. Its absorption, distribution and excretion are similar to those of calcium. After oral administration of 2g. The absolute bioavailability of strontium is 27%. Large doses of strontium can make bone mineral metabolism abnormal, and low doses of strontium can enhance the replication of pre-osteoblasts, increase the number of osteoblasts, and stimulate bone formation; at the same time, it can also reduce the activity of osteoclasts and reduce osteoclasts The number of cells reduces the rate of bone resorption. The results of studies in animals and humans are also consistent. Osteoporosis (OP) is a progressive bone disease characterized by decreased bone density (BMD) and degenerative changes in bone tissue microstructure. It is characterized by increased bone fragility and prone to fracture, the latter being most common in the spine, hip and wrist. Women stop producing estrogen that can maintain bone strength after menopause or after undergoing surgery to remove their ovaries. Therefore, primary OP is particularly common in postmenopausal or menopausal women. At present, there are two types of drugs commonly used to treat osteoporosis: one is drugs that inhibit the activity of osteoclasts and thereby inhibit bone resorption, such as bisphosphonates, estrogen, calcitonin, etc.; the second is to promote osteoblast activity To stimulate bone formation drugs, currently only one product of recombinant parathyroid hormone 1-34 is on the market, which requires injection, and the drug price is higher. |
Biological activity | Strontium Ranelate is a strontium (II) salt Ranelic acid, used for (-)-Desmethoxyverapamil binding to calcium ion channels, IC50 is 0.5 mM. |
Target | Value |
Calcium channel | 0.5 mM |
Cell Line: | Mouse calvaria (MC) cells Mouse calvaria (MC) cells |
Concentration: | 0.1 mM, 0.3 mM or 1 mM 0.1 mM, 0.3 mM or 1 mM |
Incubation Time: | 22 days 22 days |
Result: | The expression of mRNA for early osteoblast markers (ALP) was visualized by day 5, while late markers (OCN) were detectable only by day 15 and beyond. Significantly increased the mRNA expression of the osteoblastic markers ALP, BSP and OCN at day 22 of MC cell culture. |
use | is mainly used to treat and prevent osteoporosis in postmenopausal women, significantly reducing the risk of vertebral fracture and hip fracture. |